Cipralisant,213027-19-1

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Cipralisant

CAS No. : 213027-19-1

MCE 国际站：Cipralisant

产品活性：Cipralisant (GT-2331) 在体内是一种具有口服活性、低毒、有效、选择性、高亲和力的 histamine H3 receptor 的拮抗剂，在体外是 histamine H3 receptor 的激动剂，对于histamine H3 receptor，其 pK_i为 9.9，对大鼠 histamine H3 receptor 的K_i为 0.47 nM。Cipralisant 有研究注意缺陷多动障碍的潜力。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation

作用靶点：Histamine Receptor

In Vitro: Cipralisant behaves as a full agonist on adenylyl cyclase inhibition. Cipralisant (HEK cells) potently inhibits forskolin-induced cAMP accumulation, showing that Cipralisant works as a potent full histamine H3 receptor agonist. Cipralisant increases the basal [³⁵S]GTPγS binding activities in membranes from HEK cells expressing the rat histamine H3 receptor (EC₅₀, 5.6 nM).

In Vivo: Cipralisant (0.3~30 mg/kg; s.c.) enhances acquisition over five trials, reaching significance at 1 mg/kg.
Cipralisant (10 mg/kg; p.o.) completely blocks R-α-methylhistamine-induced drinking.
Cipralisant promotes wakefulness in the rat. Cipralisant potently and significantly improves performance in the repeated acquisition model, in line with its high affinity for the rat H3 receptor and good CNS penetration. Cipralisant does not appear to be as efficacious as 3 mg/kg ciproxifan at its maximally effective dose . Cipralisant behaves as a partial agonist in a rat brain synaptosome model.

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